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博莱霉素

博莱霉素用途

博莱霉素是一种糖肽抗生素。博莱霉素对一系列淋巴瘤、头颈癌和生殖细胞肿瘤具有强大的抗肿瘤活性。博莱霉素可用于癌症和化疗的研究[1][2][3][4]。

博莱霉素名称

[ CAS 号 ]:
11056-06-7

[ 中文名 ]:
博来霉素

[ 英文名 ]:
Bleocin

[中文别名 ]:

博莱霉素

[英文别名 ]:

BLM
Bleomycin
bleomicin
BLEO
BLEOMYCIN SULPHATE
BLEXANE
Bleocin
Blenoxane

博莱霉素生物活性

[ 描述 ]:

博莱霉素是一种糖肽抗生素。博莱霉素对一系列淋巴瘤、头颈癌和生殖细胞肿瘤具有强大的抗肿瘤活性。博莱霉素可用于癌症和化疗的研究[1][2][3][4]。

[ 相关类别 ]:

研究领域 >> 癌症

[体外研究]

博莱霉素(0-4 mU/mL；1 h)诱导V79细胞的双链断裂[2]。博来霉素(0-1 mU/mL；1小时)可减少S期细胞DNA的迁移[2]。博莱霉素(0-3μg/mL；1小时)诱导G2细胞染色单体畸变[3]。

[体内研究]

博莱霉素(1 mg和10μg；眶后窦注射一次)影响细胞有丝分裂,诱导肿瘤模型中的细胞凋亡[4]。动物模型：LPB和B16F0肿瘤C57Bl/6小鼠[4]剂量：1mg和10μg给药：眶后窦注射；1 mg和10μg一次。结果：两种肿瘤中有丝分裂的细胞比例降低,电脉冲传递后诱导细胞凋亡,LPB肿瘤中非典型细胞数量增加。

[参考文献]

[1]. Chen J, Stubbe J. Bleomycins: towards better therapeutics. Nat Rev Cancer. 2005;5(2):102-112.

[2]. Olive PL, et al. Detection of DNA double-strand breaks through the cell cycle after exposure to X-rays, bleomycin, etoposide and 125IdUrd. Int J Radiat Biol. 1993 Oct;64(4):349-58.

[3]. Allio T, Preston RJ. Increased sensitivity to chromatid aberration induction by bleomycin and neocarzinostatin results from alterations in a DNA damage response pathway. Mutat Res. 2000 Sep 20;453(1):5-15.

[4]. Mekid H, et al. In vivo evolution of tumour cells after the generation of double-strand DNA breaks. Br J Cancer. 2003 Jun 2;88(11):1763-71.

博莱霉素物理化学性质

[ 分子式 ]:
C₅₅H₈₅N₁₇O₂₅S₄

[ 分子量 ]:
1415.551

[ 精确质量 ]:
1414.518433

[ PSA ]:
794.66000

[ 外观性状 ]:
无色或淡黄色粉末

[ 储存条件 ]:
库房通风低温干燥

博莱霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: EC5988000

CHEMICAL NAME :: Bleomycin

CAS REGISTRY NUMBER :: 11056-06-7

LAST UPDATED :: 199706

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: Standard Draize test

ROUTE OF EXPOSURE :: Administration into the eye

SPECIES OBSERVED :: Rodent - rabbit

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 351 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - fibrosing alveolitis Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human

DOSE/DURATION :: 418 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - fibrosing alveolitis Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 168 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 168 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 35 mg/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 188 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 53 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 270 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intratracheal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 14 mg/kg

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 158 mg/kg/5W-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 88200 ug/kg/9D-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 40 mg/kg/4W-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 160 mg/kg/4W-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Lungs, Thorax, or Respiration - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 6875 ug/kg/41D-I

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair Skin and Appendages - nails

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 11 mg/kg/41D-I

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair Skin and Appendages - nails

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 44 mg/kg/30D-I

TOXIC EFFECTS :: Cardiac - cardiomyopathy including infarction Kidney, Ureter, Bladder - changes primarily in glomeruli Skin and Appendages - dermatitis, other (after systemic exposure)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 200 mg/kg

SEX/DURATION :: male 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: DNA damage

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Mutation test systems - not otherwise specified

TYPE OF TEST :: DNA inhibition

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Sister chromatid exchange

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Sister chromatid exchange

TYPE OF TEST :: DNA inhibition

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Mammal - cattle Sperm

DOSE/DURATION :: 100 mg/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 326,185,1995 *** REVIEWS *** IARC Cancer Review:Animal Limited Evidence IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,134,1987 IARC Cancer Review:Human Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 26,97,1981 IARC Cancer Review:Group 2B IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,134,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4340 No. of Facilities: 356 (estimated) No. of Industries: 1 No. of Occupations: 8 No. of Employees: 8140 (estimated) No. of Female Employees: 5555 (estimated)

博莱霉素安全信息

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
46-40

[ 安全声明 (欧洲) ]:
53-36/37-45

[ WGK德国 ]:
3

[ RTECS号 ]:
EC5991990